Method of treating cancer using selective estrogen receptor modulators
Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.
1. A method of treating an estrogen receptor positive breast cancer in a subject, wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator, the method comprising administering a composition comprising a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the composition is administered daily as a single dose or multi-dose.
2. The method of claim 1 , wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.
3. The method of claim 1 , wherein the resistance to the estrogen receptor modulator is acquired.
4. The method of claim 1 , wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM).
5. The method of claim 4 , wherein the SERM is tamoxifen, idoxifene, raloxifene or ICI 182,780.
6. The method of claim 1 , wherein the estrogen receptor modulator is an aromatase inhibitor.
7. The method of claim 6 , wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.
8. The method of claim 1 , wherein an effective amount of the compound is administered.
9. The method of claim 8 , wherein the effective amount is from about 200 mg/day to about 500 mg/day.
10. The method of claim 9 , wherein the effective amount is about 400 mg/day.
11. The method of claim 10 , wherein the compound is administered by oral administration, intravenous administration, intradermal injection, intramuscular injection or subcutaneous injection.
12. The method of claim 11 , wherein the compound is administered by oral administration.
13. The method of claim 12 , wherein the estrogen receptor modulator is tamoxifen, idoxifene, raloxifene, ICI 182,780, or an aromatase inhibitor.
14. The method of claim 13 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor), an antiestrogen, a ligand of retinoic acid or retinoxic X receptor, an antiprogestin, an antiandrogen, vitamin D or metabolite thereof, a farnesyl transferase inhibitor, a PPARα or gamma agonist and a MAP kinase inhibitor.
15. The method of claim 14 , wherein the at least one compound is a CDK4/6 inhibitor.
16. The method of claim 10 , wherein the composition is administered daily as a single dose.
17. A method of treating an estrogen receptor positive breast cancer in a subject, wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator, the method comprising administering an oral composition comprising an effective amount of a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the effective amount is from about 200 mg/day to about 500 mg/day.
18. The method of claim 17 , wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.
19. The method of claim 17 , wherein the resistance to the estrogen receptor modulator is acquired.
20. The method of claim 17 , wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM).
21. The method of claim 20 , wherein the SERM is tamoxifen, idoxifene, raloxifene or ICI 182,780.
22. The method of claim 17 , wherein the estrogen receptor modulator is an aromatase inhibitor.
23. The method of claim 22 , wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.
24. The method of claim 17 , wherein the effective amount is about 400 mg/day.
25. The method of claim 24 , wherein the estrogen receptor modulator is tamoxifen, idoxifene, raloxifene, ICI 182,780, or an aromatase inhibitor.
26. The method of claim 25 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor), an antiestrogen, a ligand of retinoic acid or retinoxic X receptor, an antiprogestin, an antiandrogen, vitamin D or metabolite thereof, a farnesyl transferase inhibitor, a PPARα or gamma agonist and a MAP kinase inhibitor.
27. The method of claim 26 , wherein the at least one compound is a CDK4/6 inhibitor.
28. The method of claim 24 , wherein the composition is administered daily as a single dose.
29. The method of claim 24 , wherein the composition is administered daily as a multi-dose.